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Kallikreins (tissue and plasma kallikrein) are a subgroup of the serine protease family.


They liberate kinins (BK and KD) from the kininogens.[1]

It also generates plasmin from plasminogen:

Fibrinolysis (simplified). Blue arrows denote stimulation, and red arrows inhibition.

Prekallikrein is the precursor of plasma kallikrein. It can only activate kinins after being activated itself by factor XII or other stimuli.


There are 15 known kallikreins: KLK1, KLK2, KLK3, KLK4, KLK5, KLK6, KLK7, KLK8, KLK9, KLK10, KLK11, KLK12, KLK13, KLK14, KLK15

Clinical significance

Kallikreins are targets of active investigation by drug researchers as possible biomarkers for cancer.[2][3]

Prostate-specific antigen (PSA; hk3, human kallikrein gene 3) and human glandular kallikrein (hK2) are used as tumor markers for prostate cancer.

See also


  1. Oikonomopoulou, K., Hansen, K.K., Saifeddine, M., Tea, I., Blaber, M., Blaber, S.I., Scarisbrick, I., Andrade-Gordon, P., Cottrell, G.S., Bunnett, N.W., Diamandis, E.P., and Hollenberg, M.D. "Proteinase-activated receptors, targets for kallikrein signaling" Journal of Biological Chemistry. 281: 32095-112, 2006.
  2. Borgono, C.A., and Diamandis, E.P. "The emerging roles of human tissue kallikreins in cancer" Nature Reviews Cancer 4: 876-90, 2004.
  3. Diamandis, E.P., and Yousef, G.M. "Human Tissue Kallikreins: A Family of New Cancer Biomarkers" Clinical Chemistry 48: 1198-1205, 2002.

External links